89421-95-4

Upstream product

• 50921-39-6 1-(4-chlorophenyl)cyclobutane-1-carboxylic acid 

Downstream Products

• 404589-70-4 2-chloro-1-[1-(4-chloro-phenyl)-cyclobutyl]-ethanone 
• 1309192-26-4 2-[1-(4-chlorophenyl)cyclobutyl]-N-[1-oxo-4-(trifluoromethyl)phthalazin-2(1H)-yl]acetamide 
• 1309195-50-3 1-(1-(4-chlorophenyl)cyclobutyl)-2-diazoethanone 
• 404893-32-9 (R)-1-[1-(4-Chloro-phenyl)-cyclobutanecarbonyl]-piperidine-3-carboxylic acid ethyl ester 

Relevant academic research and scientific papers

Amine derivatives

The present invention relates to Kv1.3 potassium channel blockers of Formula (I) and their use in the treatment of autoimmune and inflammatory diseases.

Systematic investigation of halogen bonding in protein-ligand interactions

Halogen bonding triggers activity: Increasing binding affinity was observed for a series of covalent human Cathepsin L inhibitors by exchanging an aryl ring H atom with Cl, Br, and I, which undergo halogen bonding with the C=O group of Gly61 in the S3 pocket of the enzyme. Fluorine, in contrast, strongly avoids halogen bonding (see scheme). The strong distance and angle dependence of halogen bonding was confirmed for biological systems. Copyright

POTASSIUM CHANNEL MODULATORS

Disclosed herein are KCNQ potassium channels modulators of formula (I) wherein ring Z1, R1, p, R3, and R4 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.

MULTIMEDIATOR TRANSPORTER INHIBITORS FOR USE IN TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDERS

The invention provides a class of inhibitors, packaged pharmaceuticals comprising such inhibitors, and uses of the inhibitors in treating, or the manufacturing medicaments for treating central nervous system disorders, including depression, anxiety, sleep

Discovery of 2-[1-(4-Chlorophenyl)cyclopropyl]-3-hydroxy-8- (trifluoromethyl)quinoline-4-carboxylic acid (PSI-421), a P-selectin inhibitor with improved pharmacokinetic properties and oral efficacy in models of vascular injury

Previously, we reported the discovery of PSI-697 (1a), a C-2 benzyl substituted quinoline salicylic acid-based P-selectin inhibitor. It is active in a variety of animal models of cardiovascular disease. Compound 1a has also been shown to be well tolerated and safe in healthy volunteers at doses of up to 1200 mg in a phase 1 single ascending dose study. However, its oral bioavailability was low. Our goal was to identify a back up compound with equal potency, increased solubility, and increased exposure. We expanded our structure-activity studies in this series by branching at the α position of the C-2 benzyl side chain and through modification of substituents on the carboxylic A-ring of the quinoline. This resulted in discovery of PSI-421 with marked improvement in aqueous solubility and pharmacokinetic properties. This compound has shown oral efficacy in animal models of arterial and venous injury and was selected as a preclinical development compound for potential treatment of such diseases as atherosclerosis and deep vein thrombosis.

CARBOXAMIDE DERIVATIVES AS ION CHANNEL MODULATORS

The present teachings provide compounds of Formula (I) wherein Ar, R1, R2, R3, X, p and n are defined herein. The present teachings also provide processes for producing said compounds and methods of treating a pathological condition or disorder, or alleviating a symptom thereof, using said compounds. The compounds can be useful in modulating ion channel activity including treating a variety of conditions associated with the abnormal modulation of one or more voltage-gated calcium channels.

Discovery and in vitro/in vivo studies of tetrazole derivatives as Kv1.5 blockers

A novel class of tetrazole-derived Kv1.5 blockers is disclosed. In in vitro studies, several compounds had IC50s ranging from 180 to 550 nM. In vivo studies indicated that compounds 2f and 2j increased right atrial ERP about 40% without affecting ventricular ERP.

DOPAMINE TRANSPORTER INHIBITORS FOR USE IN TREATMENT OF MOVEMENT DISORDERS AND OTHER CNS INDICATIONS

The invention provides a class of dopamine transporter inhibitors of formula (I) (DAT inhibitors) , packaged pharmaceuticals comprising such inhibitors, and their uses in treating, or the manufacturing medicaments for treating disease conditions, inlcudin

BIPHENYLOXY-ACIDS

The present invention relates generally to substituted biphenyloxy acids (such as 4'-aryl-amido-biphenyl--4(3)-yloxy-acids and 4’-aryl-amidomethyl-biphenyl-4(3)-yloxy-acids) and methods of using them.